Abstract
Novel 2,6-difuctionalized 2H-benzopyrans were synthesized and evaluated for a sphingosylphosphorylcholine(SPC) inhibitor. The synthetic 2H-benzopyrans 1c and 3a showed high potency in SPC-induced cell proliferation assay (<TEX>$IC_{50}$</TEX> < 20 nM). Neither hERG <TEX>$K^+$</TEX> channel binding (> <TEX>$10{\mu}M$</TEX>) nor CYP inhibitions (> <TEX>$10{\mu}M$</TEX>) were observed. Also, the simple structure-activity relationship (SAR) results were obtained from analysis of 2H-benzopyran derivatives 1-3 and the anti-SPC effect of 2H-benzopyran 1c was confirmed by a HUVEC tube formation assay.
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